EP1453512B8 - Derives d'acetylene possedant une activite antagoniste mglur 5 - Google Patents

Derives d'acetylene possedant une activite antagoniste mglur 5 Download PDF

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Publication number
EP1453512B8
EP1453512B8 EP02792867A EP02792867A EP1453512B8 EP 1453512 B8 EP1453512 B8 EP 1453512B8 EP 02792867 A EP02792867 A EP 02792867A EP 02792867 A EP02792867 A EP 02792867A EP 1453512 B8 EP1453512 B8 EP 1453512B8
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EP
European Patent Office
Prior art keywords
mglur
antagonistic activity
acetylene derivatives
acetylene
derivatives
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
EP02792867A
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German (de)
English (en)
Other versions
EP1453512B1 (fr
EP1453512A1 (fr
Inventor
Fabrizio Gasparini
Yves Auberson
Silvio Ofner
Terance W. Hart
Kaspar Zimmermann
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis Pharma GmbH
Novartis AG
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Publication date
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Application filed by Novartis Pharma GmbH, Novartis AG filed Critical Novartis Pharma GmbH
Priority to SI200230385T priority Critical patent/SI1453512T1/sl
Publication of EP1453512A1 publication Critical patent/EP1453512A1/fr
Publication of EP1453512B1 publication Critical patent/EP1453512B1/fr
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Publication of EP1453512B8 publication Critical patent/EP1453512B8/fr
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
EP02792867A 2001-12-04 2002-12-03 Derives d'acetylene possedant une activite antagoniste mglur 5 Expired - Lifetime EP1453512B8 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
SI200230385T SI1453512T1 (sl) 2001-12-04 2002-12-03 Derivati etina z antagonisticnim delovanjem na MGLUR 5

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0128996 2001-12-04
GBGB0128996.6A GB0128996D0 (en) 2001-12-04 2001-12-04 Organic compounds
PCT/EP2002/013670 WO2003047581A1 (fr) 2001-12-04 2002-12-03 Derives d'acetylene possedant une activite antagoniste mglur 5

Publications (3)

Publication Number Publication Date
EP1453512A1 EP1453512A1 (fr) 2004-09-08
EP1453512B1 EP1453512B1 (fr) 2006-05-31
EP1453512B8 true EP1453512B8 (fr) 2006-07-19

Family

ID=9926969

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02792867A Expired - Lifetime EP1453512B8 (fr) 2001-12-04 2002-12-03 Derives d'acetylene possedant une activite antagoniste mglur 5

Country Status (32)

Country Link
US (4) US7348353B2 (fr)
EP (1) EP1453512B8 (fr)
JP (2) JP4176020B2 (fr)
KR (2) KR100959204B1 (fr)
CN (2) CN100430059C (fr)
AR (2) AR037682A1 (fr)
AT (1) ATE327755T1 (fr)
AU (1) AU2002358585B2 (fr)
BR (1) BR0214666A (fr)
CA (1) CA2466560C (fr)
CO (1) CO5590929A2 (fr)
CY (1) CY1105460T1 (fr)
DE (1) DE60211944T2 (fr)
DK (1) DK1453512T3 (fr)
EC (1) ECSP045139A (fr)
EG (1) EG24936A (fr)
ES (1) ES2263842T3 (fr)
GB (1) GB0128996D0 (fr)
HK (1) HK1071510A1 (fr)
HU (1) HU229429B1 (fr)
IL (1) IL161990A0 (fr)
MX (1) MXPA04005456A (fr)
MY (1) MY137774A (fr)
NO (1) NO327005B1 (fr)
NZ (1) NZ533266A (fr)
PE (1) PE20030640A1 (fr)
PL (1) PL212996B1 (fr)
PT (1) PT1453512E (fr)
RU (1) RU2341515C2 (fr)
TW (1) TWI328578B (fr)
WO (1) WO2003047581A1 (fr)
ZA (1) ZA200403713B (fr)

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0128996D0 (en) * 2001-12-04 2002-01-23 Novartis Ag Organic compounds
US7772188B2 (en) 2003-01-28 2010-08-10 Ironwood Pharmaceuticals, Inc. Methods and compositions for the treatment of gastrointestinal disorders
GB0325956D0 (en) * 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
US20080125403A1 (en) 2004-04-02 2008-05-29 Merck & Co., Inc. Method of Treating Men with Metabolic and Anthropometric Disorders
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0508314D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508318D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0514296D0 (en) * 2005-07-12 2005-08-17 Novartis Ag Organic compounds
MX2009002684A (es) * 2006-09-11 2009-06-05 Novartis Ag Derivados de acido nicotinico como moduladores de receptores de glutamato metabotropico.
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
WO2008151257A2 (fr) 2007-06-04 2008-12-11 Synergy Pharmaceuticals Inc. Agonistes de guanylase cyclase utiles pour le traitement de troubles gastro-intestinaux, d'inflammation, de cancer et d'autres troubles
SG185293A1 (en) * 2007-10-12 2012-11-29 Novartis Ag Organic compounds
AU2012254934B2 (en) * 2007-10-12 2013-10-17 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease
AU2009256157B2 (en) 2008-06-04 2014-12-18 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
AU2009265760B2 (en) * 2008-06-30 2013-07-18 Novartis Ag Combinations comprising mGluR modulators for the treatment of parkinson's disease
MY151183A (en) * 2008-08-12 2014-04-30 Novartis Ag Processes for the preparation of 4-oxo-octahydro-indole-1-carbocyclic acid methyl ester and derivatives thereof
US8334287B2 (en) 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
EP2959902A1 (fr) 2009-07-23 2015-12-30 Novartis AG Utilisation de dérivés d'azabicycloalkyle pour la prévention ou le traitement de l'ataxie
TWI558398B (zh) 2009-09-22 2016-11-21 諾華公司 菸鹼乙醯膽鹼受體α７活化劑之用途
EP2490691A1 (fr) 2009-10-20 2012-08-29 Novartis AG Utilisation de 1h-quinazoline-2,4-diones
SG184458A1 (en) * 2010-04-30 2012-11-29 Novartis Ag Predictive markers useful in the treatment of fragile x syndrome (fxs)
KR20130098181A (ko) 2010-06-24 2013-09-04 노파르티스 아게 1ｈ-퀴나졸린-2,4-디온의 용도
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
EP2655326A1 (fr) * 2010-12-20 2013-10-30 Novartis AG Esters d'acides 4-(hétéro)aryl-éthynyl-octahydro-indole-1-carboxyliques
WO2012101058A1 (fr) 2011-01-24 2012-08-02 Novartis Ag Dérivés de 4-tolyl-éthynyl-octahydro-indole-1-ester
CA2825142A1 (fr) 2011-01-27 2012-08-02 Novartis Ag Utilisation d'activateurs du recepteur nicotinique de l'acetylcholine alpha 7
EP2685977A1 (fr) 2011-03-18 2014-01-22 Novartis AG Combinaisons d'activateurs des récepteurs nicotiniques à l'acétylcholine alpha 7 et d'antagonistes des mglur5 destinées à être utilisées dans la dyskinésie induite par la dopamine dans la maladie de parkinson
MX2014002693A (es) 2011-09-07 2014-06-04 Novartis Ag Uso de 1h-quinazolina-2,4-dionas para usarse en la prevencion o el tratamiento de epilepsia fotosensible.
WO2013131981A1 (fr) 2012-03-08 2013-09-12 Novartis Ag Marqueurs de prédiction utiles dans le diagnostic et le traitement du syndrome de l'x fragile (fxs)
GB201215033D0 (en) 2012-08-23 2012-10-10 Novartis Ag Diazepinone derivatives
WO2014111751A1 (fr) 2013-01-15 2014-07-24 Novartis Ag Utilisation d'agonistes du récepteur nicotinique alpha 7 pour le traitement de la narcolepsie
MX2015009153A (es) 2013-01-15 2016-03-04 Novartis Ag Uso de agonistas del receptor nicotinico de acetilcolina alfa 7.
WO2014151206A1 (fr) 2013-03-15 2014-09-25 Synergy Pharmaceuticals Inc. Agonistes de la guanylate cyclase et leurs utilisations
AU2014235209B2 (en) 2013-03-15 2018-06-14 Bausch Health Ireland Limited Guanylate cyclase receptor agonists combined with other drugs
WO2014197720A2 (fr) 2013-06-05 2014-12-11 Synergy Pharmaceuticals, Inc. Agonistes ultra-purs de guanylate cyclase c, leur procédé de production et d'utilisation
TN2015000498A1 (en) 2013-06-12 2017-04-06 Novartis Ag Modified release formulation
CN105669686B (zh) * 2014-11-19 2018-08-03 上海合全药业股份有限公司 一种6-(叔丁氧羰基)八氢呋喃[2,3-c]吡啶-4-羧酸的合成方法
WO2019025931A1 (fr) 2017-07-31 2019-02-07 Novartis Ag Utilisation de mavoglurant dans la réduction de l'utilisation de cocaïne ou dans la prévention d'une rechute dans l'utilisation de cocaïne
EP3661501A1 (fr) 2017-07-31 2020-06-10 Novartis AG Utilisation de mavoglurant dans la réduction de l'utilisation d'alcool ou dans la prévention de rechute dans l'utilisation d'alcool
BR112021014342A2 (pt) 2019-01-29 2021-09-21 Novartis Ag Uso de um antagonista mglur5 para tratar tolerância a analgésico opioide
MX2023000664A (es) 2020-07-17 2023-02-27 Novartis Ag Uso de antagonistas de mglur5.
WO2022123482A1 (fr) 2020-12-11 2022-06-16 Novartis Ag Utilisation d'antagonistes de mglur5 pour le traitement de la dépendance à l'amphétamine
CA3204360A1 (fr) 2020-12-14 2022-06-23 Novartis Ag Utilisation d'antagonistes de mglur5 pour traiter un trouble lie aux jeux d'argent

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2741009A1 (de) * 1976-09-22 1978-03-23 Sandoz Ag 4-styryl-4-indolinol-derivate, ihre verwendung und herstellung
DE2802833A1 (de) 1978-01-23 1979-07-26 Sandoz Ag 4-styryl-4-indolinol-derivate, ihre verwendung und herstellung
US5264456A (en) 1989-12-29 1993-11-23 Allergan, Inc. Acetylenes disubstituted with a furyl group and a substituted phenyl group having retinoid like activity
US5284957A (en) 1992-09-03 1994-02-08 Eli Lilly And Company Excitatory amino acid receptor antagonists
US5593994A (en) 1994-09-29 1997-01-14 The Dupont Merck Pharmaceutical Company Prostaglandin synthase inhibitors
DE69634822T2 (de) 1995-08-22 2006-04-27 Japan Tobacco Inc. Amid-verbindungen und ihre anwendung
AU3102697A (en) 1996-06-19 1998-01-07 Rhone-Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
DE69915472T2 (de) 1998-06-04 2004-08-19 Kumiai Chemical Industry Co., Ltd. Phenylacetylenderivate und bakterizide für landwirtschaft und gartenbau
PT1117403E (pt) 1998-10-02 2004-04-30 Sibia Neurosciences Inc Antagonistas de mglurs para o tratamento da dor e ansiedade
DE60032905T2 (de) 1999-07-06 2007-10-18 Eli Lilly And Co., Indianapolis Selektive iglur5 rezeptorantagonisten zur behandlung der migräne
GB0007108D0 (en) 2000-03-23 2000-05-17 Novartis Ag Organic compounds
NZ526003A (en) 2000-10-20 2005-09-30 Biocryst Pharm Inc Biaryl compounds as serine protease inhibitors
IL155999A0 (en) 2000-12-04 2003-12-23 Hoffmann La Roche Phenylethenyl or phenylethinyl derivatives as glutamate receptor antagonists
GB0103045D0 (en) * 2001-02-07 2001-03-21 Novartis Ag Organic Compounds
US7138404B2 (en) 2001-05-23 2006-11-21 Hoffmann-La Roche Inc. 4-aminopyrimidine derivatives
HUP0402344A2 (hu) 2001-12-04 2005-02-28 F. Hoffmann-La Roche Ag Helyettesített 2-amino-cikloalkán-karboxamidok, felhasználásuk cisztein-proteáz-inhibitorként, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
TW200303309A (en) 2001-12-04 2003-09-01 Bristol Myers Squibb Co Novel n-[4-(1h-imidazol-1-yl)-2-fluorophenyl]-3-trifluoromethyl)-1h-pyrazole-5-carboxamides as factor Xa inhibitors
GB0128996D0 (en) 2001-12-04 2002-01-23 Novartis Ag Organic compounds

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PL368739A1 (en) 2005-04-04
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JP2005514381A (ja) 2005-05-19
PT1453512E (pt) 2006-10-31
US20080146647A1 (en) 2008-06-19
CN1592623A (zh) 2005-03-09
CA2466560C (fr) 2010-07-27
CN101366714B (zh) 2014-09-17
AR088921A2 (es) 2014-07-16
EP1453512B1 (fr) 2006-05-31
DE60211944D1 (de) 2006-07-06
MY137774A (en) 2009-03-31
US20130331568A1 (en) 2013-12-12
JP2008303226A (ja) 2008-12-18
DE60211944T2 (de) 2007-05-16
AR037682A1 (es) 2004-12-01
ECSP045139A (es) 2004-07-23
HUP0402191A3 (en) 2010-03-29
AU2002358585B2 (en) 2006-01-19
RU2341515C2 (ru) 2008-12-20
US20050065191A1 (en) 2005-03-24
DK1453512T3 (da) 2006-08-28
MXPA04005456A (es) 2004-10-11
CA2466560A1 (fr) 2003-06-12
US7348353B2 (en) 2008-03-25
JP5036648B2 (ja) 2012-09-26
KR20100020044A (ko) 2010-02-19
HU229429B1 (en) 2013-12-30
WO2003047581A1 (fr) 2003-06-12
IL161990A0 (en) 2005-11-20
NO327005B1 (no) 2009-04-06
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US20120010263A1 (en) 2012-01-12
US8536229B2 (en) 2013-09-17
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HK1071510A1 (en) 2005-07-22
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GB0128996D0 (en) 2002-01-23
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ZA200403713B (en) 2005-10-26
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EP1453512A1 (fr) 2004-09-08
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